ES2012648A6 - 1,4-benzoxazine and 1,4-benzothiazine derivatives and process for their preparation. - Google Patents

1,4-benzoxazine and 1,4-benzothiazine derivatives and process for their preparation.

Info

Publication number
ES2012648A6
ES2012648A6 ES8900519A ES8900519A ES2012648A6 ES 2012648 A6 ES2012648 A6 ES 2012648A6 ES 8900519 A ES8900519 A ES 8900519A ES 8900519 A ES8900519 A ES 8900519A ES 2012648 A6 ES2012648 A6 ES 2012648A6
Authority
ES
Spain
Prior art keywords
alkyl
hydrogen
independently
trihalo
nitro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES8900519A
Other languages
Spanish (es)
Inventor
Mario Verasi
Piero Melloni
M Antonietta Cervini
Alberto Bonsignori
Roberto Commisso
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Italia SRL
Original Assignee
Farmitalia Carlo Erba SRL
Carlo Erba SpA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Farmitalia Carlo Erba SRL, Carlo Erba SpA filed Critical Farmitalia Carlo Erba SRL
Publication of ES2012648A6 publication Critical patent/ES2012648A6/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/141,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/161,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

The present invention relates to compounds having formula (I), wherein X represents -O- or -S- each of R and R1, independently, is hydrogen, halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, amino, nitro or trihalo-C1-C6 alkyl each of R2 and R3, independently, is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or phenyl-C1-C6 alkyl or R2 and R3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen each of R4 and R5, independently, is hydrogen, halogen, nitro, amino or trihalo-C1-C6 alkyl and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.
ES8900519A 1988-02-15 1989-02-14 1,4-benzoxazine and 1,4-benzothiazine derivatives and process for their preparation. Expired - Lifetime ES2012648A6 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB888803419A GB8803419D0 (en) 1988-02-15 1988-02-15 1 4-benzoxazine & 1 4-benzothiazine derivatives & process for their preparation

Publications (1)

Publication Number Publication Date
ES2012648A6 true ES2012648A6 (en) 1990-04-01

Family

ID=10631705

Family Applications (1)

Application Number Title Priority Date Filing Date
ES8900519A Expired - Lifetime ES2012648A6 (en) 1988-02-15 1989-02-14 1,4-benzoxazine and 1,4-benzothiazine derivatives and process for their preparation.

Country Status (19)

Country Link
US (1) US5084454A (en)
EP (1) EP0359790B1 (en)
JP (1) JPH02503200A (en)
KR (1) KR900700468A (en)
CA (1) CA1327575C (en)
DE (1) DE68910451T2 (en)
DK (1) DK506289D0 (en)
ES (1) ES2012648A6 (en)
FI (1) FI894798A0 (en)
GB (1) GB8803419D0 (en)
GR (1) GR1000373B (en)
HU (1) HU204517B (en)
IE (1) IE890464L (en)
IL (1) IL89035A (en)
NZ (1) NZ227739A (en)
PT (1) PT89715B (en)
RU (1) RU1826968C (en)
WO (1) WO1989007596A1 (en)
ZA (1) ZA891107B (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5240927A (en) * 1992-05-19 1993-08-31 Hoechst-Roussel Pharmaceuticals Incorporated Benzo[β]thiophen-3-yl piperazines as antipsychotic agents
FR2702477B1 (en) * 1993-03-08 1995-04-28 Synthelabo Benzoxazine derivatives, their preparation and their therapeutic application.
US5691323A (en) * 1995-05-12 1997-11-25 Merck & Co., Inc. Muscarine antagonists
US6162803A (en) * 1998-04-08 2000-12-19 American Home Products Corp. Indol-3-yl-cyclohexyl amine derivatives for the treatment of depression
JP3201998B2 (en) * 1998-12-16 2001-08-27 サムソン ジェネラル ケミカルズ カンパニー リミテッド Method for producing (S) -benzoxazine derivative and method for racemizing (R) -benzoxazine derivative
TW546299B (en) * 1999-01-07 2003-08-11 Wyeth Corp 3,4-dihydro-2H-benzo[1,4]oxazinyl-methyl-[3-(1H-indol-3-yl)-alkyl]-amines
US6313114B1 (en) 1999-01-07 2001-11-06 American Home Products Corp 3,4-Dihydro-2H-benzo[1,4]oxazinyl-methyl)-[3-(1H-indol-3yl)-alkyl]- amines
AU2494300A (en) * 1999-01-07 2000-07-24 American Home Products Corporation 3,4-dihydro-2h-benzo(1,4)oxazine derivatives
US6221863B1 (en) 1999-01-07 2001-04-24 American Home Products Corp. 3,4-dihydro-2H-benzo[1,4]oxazine derivatives
US6586433B2 (en) 1999-09-23 2003-07-01 Pharmacia Corporation Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
US6677341B2 (en) 1999-09-23 2004-01-13 Pharmacia Corporation (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
CA2547764A1 (en) 2003-12-09 2005-06-30 F.Hoffmann-La Roche Ag Benzoxazine derivatives and uses thereof
CN101836993B (en) 2010-05-20 2011-06-22 山东大学 Application of 2,3-dihydrogen-3-hydroxymethyl-6-amino-[1,4]-benzoxazine in preparing medicaments for inducing embryonic stem cells to differentiate towards vascular endothelial cells

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3058980A (en) * 1962-10-16 Substitution products of benzo-
GB2080791B (en) * 1980-06-19 1984-02-22 Erba Farmitalia 1,4-benzoxazines
GB8511526D0 (en) * 1985-05-07 1985-06-12 Hoechst Uk Ltd 1 4 benzodioxin & 1 4 benzoxazine derivatives
EP0233728A1 (en) * 1986-02-11 1987-08-26 Takeda Chemical Industries, Ltd. 1,4-Benzoxazine derivatives their production and use

Also Published As

Publication number Publication date
IL89035A0 (en) 1989-08-15
IE890464L (en) 1989-08-15
US5084454A (en) 1992-01-28
HU204517B (en) 1992-01-28
RU1826968C (en) 1993-07-07
PT89715A (en) 1989-10-04
HUT56354A (en) 1991-08-28
PT89715B (en) 1994-03-31
GR1000373B (en) 1992-06-30
KR900700468A (en) 1990-08-13
IL89035A (en) 1994-05-30
DE68910451D1 (en) 1993-12-09
GB8803419D0 (en) 1988-03-16
EP0359790A1 (en) 1990-03-28
NZ227739A (en) 1990-08-28
FI894798A0 (en) 1989-10-10
DK506289A (en) 1989-10-12
DK506289D0 (en) 1989-10-12
WO1989007596A1 (en) 1989-08-24
ZA891107B (en) 1989-10-25
CA1327575C (en) 1994-03-08
HU891441D0 (en) 1990-01-28
EP0359790B1 (en) 1993-11-03
JPH02503200A (en) 1990-10-04
DE68910451T2 (en) 1994-03-03

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